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Comparative study between chloramine-T and iodogen to prepare radioiodinated etodolac for inflammation imaging

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Abstract

This study describes a fast and efficient method for radiolabeling of etodolac with iodine-125 [125I], where both chloramine-T and iodogen were used as oxidizing agents. The labeling reaction was carried out via electrophilic substitution of hydrogen atom with the iodonium cation I+. The labeling yield was found to be influenced by different factors such as drug concentration, pH of the reaction mixtures, different oxidizing agents, reaction time, temperature and different organic media. The radiochemical yield (RCY) was determined by TLC system using methylene chloride:ethyl acetate (3:7 v/v) as a developing solvent and by electrophoresis using cellulose acetate moistened with 0.02 M phosphate buffer pH 7. The maximum radiochemical yield of [125I]Etodolac (87.7%) was obtained. Labeled etodolac shows a good localization in inflamed muscle. It excretes mainly via kidney and to some via liver.

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Authors and Affiliations

  1. Cyclotron Project, Nuclear Research Center, Atomic Energy Authority, P.O. Box. 13759, Cairo, Egypt

    H. Hussien & U. Seddik

  2. Labeled Compound Department, Hot Labs Center, Atomic Energy Authority, Cairo, Egypt

    A. M. Amin

  3. Faculty of Science, Zagazig University, Zagazig, Egypt

    A. A. Goud & R. EL-Sheikh

Authors
  1. H. Hussien
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  2. A. A. Goud
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  3. A. M. Amin
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  4. R. EL-Sheikh
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  5. U. Seddik
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Correspondence to H. Hussien.

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Hussien, H., Goud, A.A., Amin, A.M. et al. Comparative study between chloramine-T and iodogen to prepare radioiodinated etodolac for inflammation imaging. J Radioanal Nucl Chem 288, 9–15 (2011). https://doi.org/10.1007/s10967-010-0967-9

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  • DOI: https://doi.org/10.1007/s10967-010-0967-9

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